Synthesis and antibacterial activity of nitroaryl thiadiazole-gatifloxacin hybrids.
A number of gatifloxacin analogues containing a nitroaryl-1,3,4-thiadiazole moiety attached to the piperazine ring at C-7 position were prepared and evaluated as antibacterial agents against a panel of gram-positive and gram-negative bacteria. Among synthesized compounds, nitrofuran analog 6a exhibited more potent inhibitory activity against gram-positive bacteria including Staphylococcus epidermidis (MIC=0.0078 microg/mL), Bacillus subtilis (MIC=0.0039 microg/mL), Enterococcus faecalis (MIC=0.125 microg/mL) and Micrococcus luteus (MIC=0.125 microg/mL), with respect to other synthesized compounds and reference drug gatifloxacin. The target compounds were also assessed for their cytotoxic activity against normal mouse fibroblast (NIH/3T3) cells using MTT assay. The results indicated that these compounds exhibit antibacterial activity at non-cytotoxic concentrations.
Jazayeri
Seyyedehsamira
S
Department of Chemistry, Islamic Azad University, Tehran North-Branch, Tehran, Iran.
Moshafi
Mohammad Hassan
MH
Firoozpour
Loghman
L
Emami
Saeed
S
Rajabalian
Saeed
S
Haddad
Mitra
M
Pahlavanzadeh
Farahnaz
F
Esnaashari
Manzarbanoo
M
Shafiee
Abbas
A
Foroumadi
Alireza
A
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077734:Gatifloxacin; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008826:Microbial Sensitivity Tests; D041681:NIH 3T3 Cells; D013055:Spectrophotometry, Infrared; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D013830:Thiadiazoles; D000077734:Gatifloxacin